Glutaminase-IN-1
Names
[ CAS No. ]:
2247127-79-1
[ Name ]:
Glutaminase-IN-1
Biological Activity
[Description]:
Glutaminase-IN-1, a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 shows improved cellular uptake and antitumor activity.
[Related Catalog]:
[Target]
IC50: 1 nM (KGA)[1].
[In Vitro]
Glutaminase-IN-1 (CPD20), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 shows improved cellular uptake and antitumor activity. The IC50 values of Glutaminase-IN-1 are 17 nM, 6.78 μM, 19 nM and 9 nM in A549, H2, Caki-1 and HCT116 cell lines, respectively. Glutaminase-IN-1 has better KGA inhibitory activity than the corresponding BPTES and CB839[1].
[In Vivo]
Glutaminase-IN-1(10 mg/kg, i.h.) reduced the size and weight of the HCT116 tumor, and statistical analysis showed that the 40% reduction in tumor weight by CPD20 is statistically significant. Glutaminase-IN-1 could statistically significantly prolong the survival of H22-bearing mice[1].
[References]
[Related Small Molecules]
Captisol
|
Cyclosporin A
|
H2DCFDA
|
0MPTP hydrochloride
|
GW4869
|
Etomoxir
|
TD139
|
Mitoquinone mesylate
|
GSK2795039
|
JC-1
|
BAPTA-AM
|
AP 20187
|
Setanaxib (GKT137831)
|
D-Luciferin
|
Crotaline
Chemical & Physical Properties
[ Molecular Formula ]:
C26H24F3N7O3Se
[ Molecular Weight ]:
618.47
[ Storage condition ]:
2-8℃